| 摘要 |
The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor, of the formula <CHEM> in which R is C1-C4 alkyl, C3-C4 alkenyl, or cyclopropylmethyl; R3 is hydrogen; or R and R3 taken together are a divalent group of the formula -CH2CH2CH2-; R1 is hydrogen, C1-C4 alkyl, C3-C4 alkenyl, cyclopropylmethyl, aryl(C1-C4-alkyl), -COR4, -(CH2)nS(C1-C4 alkyl) or -(CH2)nCONR5R6; n is an integer from 1 to 4; R4 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, or phenyl; R5 and R6 are independently hydrogen, C1-C4 alkyl, or C3-C7 cycloalkyl with the proviso that when one of R5 or R6 is cycloalkyl the other is hydrogen; X is -CH2-, -O-, -S-, <CHEM> A is <CHEM> R2 is C1-C8 alkyl, substituted C1-C8 alkyl, C2-C4 alkenyl, aryl, substituted aryl, aryl(C1-C4-alkyl), substituted aryl(C1-C4 alkyl), C3-C7 cycloalkyl-substituted methyl, or C3-C7 cycloalkyl; and pharmaceutically acceptable acid addition salts thereof. |
